DELIVERY OF LOPERAMIDE ACROSS THE BLOOD-BRAIN-BARRIER WITH POLYSORBATE 80-COATED POLYBUTYLCYANOACRYLATE NANOPARTICLES

Purpose, The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid agonist loperamide acro ss the blood-brain barrier was investigated. The analgesic effect afte r i.v. injection of the preparations was used to indicate drug transpo rt through this barrier. Methods. Loperamide was incorporated into PBC A nanoparticles. Drug-containing nanoparticles were coated with polyso rbate 80 and injected intravenously into mice. Analgesia was then meas ured by the tail-flick test. Results. Intravenous injection of the par ticulate formulation resulted in a long and significant analgesic effe ct. A polysorbate 80 loperamide solution induced a much less pronounce d and very short analgesia. Uncoated nanoparticles loaded with loperam ide were unable to produce analgesia. Conclusions. Polysorbate 80-coat ed PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain.